6-Substituted adenosines are known. Additionally, variations at the 5' position on a ribose substituent of adenosines are known.
For example, DT 2632951 described in Derwent Abstract No. 11515Y/07 U.S. Pat. No. 4,122,172 described in Derwent Abstract No. 76155X/41 disclose a compound of the formula XX wherein Z is defined as various substituents attached at the 5' ribose position of an adenosine through a carbonyl. DT 2730-846 and DT 2632-950 are more specific disclosures to variations of adenosines generally of formula XX. Numerous other references disclose various 5' substituents having essentially the formula XX.
6-Substituted adenosines having various 5' substituents include the compounds of formula XXI (U.S. Pat. No. 3,830,795-Derwent Abstract No. 62864V35), XXII (U.S. Pat. No. 3,931,401-Derwent Abstract No. 05487X/03), XXIII where R.sup.IV and R.sup.V may be hydrogen, acyl or together a diacyl residue of an aliphatic or aromatic dicarboxylic acid (DT 2606532-Derwent AbstractNo. 6731X/36), XXIV where R.sup.VI, may be hydrogen or allyl (U.S. Pat. No. 3,914,414 and 3,914,415-Derwent Abstract No. 74014W/44 and 74015W/44 respectively). Similarly, EP Application 0066918 discloses 6-substituted amino compounds wherein the 6-substitutions are 1-4C alkyl or phenyl of formula XXV having Z' defined as CONR.sup.IV R.sup.V or CO.sub.2 R.sup.V.
Specifically, U.S. Application No. (Case 3254C1), U.S. Application No. (Case 3252C1), and U.S. Application No. (Case 3250C1) disclose 5' deoxy, 5' deoxy-5'-methylthio, or 5'-deoxy-5'-halogen variations of 6-Substituted adenosines. Further, U.S. Application No. 625,450 filed June 28, 1984 discloses N.sup.6 substituted and 5'-N-substituted Carboxamidoadenosine derivatives as cardiac vasodilators. All of these U.S. applications are hereby incorporated by reference.
U.S. Pat. No. 3852268 described in Derwent Abstract No. 88536V/51 and U.S. Pat. No. 3853846 described in Derwent Abstract No. 90059V/52 disclose inosines having various 5' substituents.
Further, references such as U.S. Pat. No. 3922,261, German Application 2,402,804 and U.S. Pat. No. 4,501,735 disclose various 6-benzocycloalkyl adenosines. U.S. Pat. No. 3,502,649 discloses 6-arylisopropyladenosine and U.S. Serial No. 519,284 or a continuation thereof discloses 6-diarylalkyladenosine. Also disclosed in U.S. Pat. No. 3,590,029 are N-6-cycloalkyladenosines. However, none of these references teach a 5' variation on the ribose moiety of the disclosed adenosines.
Therefore, none of the above noted references disclose the adenosines of the present invention. Particularly, there is no teaching to the combination of substituents at the 6 and 5' positions of the present novel adenosines. Further, no teaching in the above noted references shows preparation for the present invention adenosines having the N6 substituted-5'-substituted moieties defined hereinafter. ##STR1##